中文名 | UNC0224 |
英文名 | UNC0224 |
别名 | G9A抑制剂(UNC0224) 7-[3-(二甲基氨基)丙氧基]-2-(六氢-4-甲基-1H-1,4-二氮杂卓-1-基)-6-甲氧基-N-(1-甲基-4-哌啶基)-4-喹唑啉胺 |
英文别名 | CS-1635 UNC0224 UNC 0224 UNC-0224 UNC0224 UNC 0224 N-Debenzyl-N-Methyl-O-deMethyl-O-(3-diMethylaMinopropyl)-BIX 01294 7-[3-(dimethylamino)propoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine 7-[3-(Dimethylamino)propoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine 4-QuinazolinaMine, 7-[3-(diMethylaMino)propoxy]-2-(hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6-Methoxy-N-(1-Methyl-4-piperidinyl)- |
CAS | 1197196-48-7 |
化学式 | C26H43N7O2 |
分子量 | 485.67 |
密度 | 1.141±0.06 g/cm3(Predicted) |
沸点 | 641.0±65.0 °C(Predicted) |
溶解度 | 溶于DMSO |
酸度系数 | 9.34±0.70(Predicted) |
存储条件 | 2-8°C |
体外研究 | In G9a ECSD and CLOT assays, the IC 50 values of 43 nM and 57 nM for UNC0224 (Compound 10), respectively. In GLP ECSD and CLOT assays, the IC 50 values of 50 nM and 58 nM for UNC0224, respectively. In ITC experiments, the K d value of UNC0224 to the G9a protein is 23 nM. |
参考资料 展开查看 | 1: Liu F, Chen X, Allali-Hassani A, Quinn AM, Wigle TJ, Wasney GA, Dong A, Senisterra G, Chau I, Siarheyeva A, Norris JL, Kireev DB, Jadhav A, Herold JM, Janzen WP, Arrowsmith CH, Frye SV, Brown PJ, Simeonov A, Vedadi M, Jin J. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57. doi: 10.1021/jm100478y. PubMed PMID: 20614940; PubMed Central PMCID: PMC2920043. 2: Liu F, Chen X, Allali-Hassani A, Quinn AM, Wasney GA, Dong A, Barsyte D, Kozieradzki I, Senisterra G, Chau I, Siarheyeva A, Kireev DB, Jadhav A, Herold JM, Frye SV, Arrowsmith CH, Brown PJ, Simeonov A, Vedadi M, Jin J. Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J Med Chem. 2009 Dec 24;52(24):7950-3. doi: 10.1021/jm901543m. PubMed PMID: 19891491; PubMed Central PMCID: PMC2825141. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.059 ml | 10.295 ml | 20.59 ml |
5 mM | 0.412 ml | 2.059 ml | 4.118 ml |
10 mM | 0.206 ml | 1.03 ml | 2.059 ml |
5 mM | 0.041 ml | 0.206 ml | 0.412 ml |
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